NO-SCA

Active material: Drotaverine
When ATH: A03AD02
CCF: Myotropic antispasmodic
ICD-10 codes (testimony): K25, K26, K29, K31.3, K52, K81.0, K81.1, K82.8, K83.0, N10, N11, N20, N21, N23, N30, N94.4, N94.5, O62, R10.4, R51
When CSF: 02.15.08
Manufacturer: CHINOIN Pharmaceutical and Chemical Works Co. Ltd. (Hungary)

Pharmaceutical form, composition and packaging

◊ Pills round, lenticular, with greenish yellow or orange tint, labeled “spa” on one side.

Excipients: magnesium stearate, talc, polyvidone, corn starch, lactose monohydrate.

10 PC. – blisters (2) – packs cardboard.
60 PC. – polypropylene bottles with dispenser “push-top” (1) – packs cardboard.
100 PC. – vials made of polypropylene (1) – packs cardboard.

Solution for in / and the / m clear, greenish yellow.

Excipients: sodium metabisulfite, ethanol 96%, water d / and.

2 ml – vials of dark glass (5) – packings Valium plastic (1) – packs cardboard.
2 ml – vials of dark glass (5) – packings Valium plastic (5) – packs cardboard.

Pharmacological action

Antispasmodics. Drotaverinum - isoquinoline derivative, which exerts a spasmolytic effect on smooth muscle by inhibiting the enzyme phosphodiesterase 4 (PDE4). Inhibition of the enzyme PDE4 leads to elevated concentrations of cAMP, that inactivates myosin light chain kinase (MLCK), what, in turn, leading to smooth muscle relaxation.

Drotaverine inhibits the enzyme PDE4 inhibition in vitro without PDE3 and PDE5 isozyme. Apparently, PDE4 is functionally very important to reduce the contractility of the smooth muscle, therefore selective PDE4 inhibitors may be effective in the treatment of hyperkinetic disorders and diseases, associated with spastic states of the gastrointestinal tract.

Enzyme, hydrolyzes cAMP in smooth muscle cells of the myocardium and blood vessels, isoenzyme is mainly FDE3, which explains the high efficiency drotaverine like antispasmodic with no pronounced effect on the cardiovascular system and serious cardiovascular adverse reactions. The drug is effective in smooth muscle spasms like nervous, and muscular etiologies. Regardless of the type of autonomic innervation drotaverine effect on the smooth muscles of the digestive tract, Biliary, and genitourinary and vascular systems. Thanks vasodilator action Nospanum^® improves blood circulation.

Pharmacokinetics

Absorption and distribution

If ingestion and parenteral administration drotaverine rapidly and completely absorbed. C_max It reached within 45-60 m. Bound to plasma proteins (alpha-albumin, alpha- and beta-globulins).

Metabolism and excretion

It is metabolized in the liver. T_1/2 – 16-22 no. Through 72 h drotaverine excreted mainly as metabolites, 50% – urine, 30% – with feces.

Testimony

- Smooth muscle spasms, associated with diseases of the biliary tract: cholelithiasis, cholecystitis, periholetsistit, kholangit, papillitis;

- Spasms of smooth muscles of the urinary system: urolithiasis disease, pyelitis, cystitis, tenesmus bladder;

- During physiological birth – shortening phase of cervical dilatation and thereby reducing the total duration of labor (for a solution for I / O, and the / m).

As an adjuvant therapy:

- Spasm of smooth muscles of the digestive tract: gastric ulcer and duodenal ulcer, gastritis, spasm of the cardia and pylorus, enteritis, colitis, accompanied by constipation and flatulence;

- Tension headaches (orally);

- Gynecological diseases (dysmenorrhoea);

- Strong labor pains (for a solution for I / O, and the / m).

When used as an adjuvant drug is administered parenterally if you can not use tablets.

Dosage regimen

Adults when administered the recommended daily dose is 120-240 mg (in 2-3 admission); children dose adjusted, depending on the age, for children from 1 to 6 years – 40-120 mg (in 2-3 admission); in age 6 years – 80-200 mg (in 2-5 receptions).

The average daily intake for the / m adults is 40-240 mg (divided by 1-3 administration / day). At acute colic (kidney or bile) preparation is administered in / dose 40-80 mg.

To shortening phase of cervical dilatation during physiological birth injected i / m 40 mg, that an unsatisfactory effect may be repeated 1 times during 2 no.

Side effect

From the digestive system: rarely - nausea, constipation.

CNS: seldom - a headache, dizziness, insomnia.

Cardio-vascular system: rarely - heart palpitations; very rarely - hypotension.

Other: very rarely - allergic reactions (when administered parenterally, especially in patients with hypersensitivity to bisulfite).

Contraindications

- Severe renal insufficiency;

- Severe hepatic impairment;

- Severe heart failure (low cardiac output syndrome);

- Children up to age 1 year (Pill);

- Hypersensitivity to drotaverine or to any excipient formulation (in particular to sodium metabisulphite – for a solution for I / O, and the / m).

FROM caution use in patients with hypotension. The on / in the introduction of the drug the patient should be in a prone position because of the danger of collapse.

Pregnancy and lactation

Drotaverine not teratogenic and embryotoxic action. However, use of the drug is recommended only after careful weighing of the expected benefits and the ratio of possible risk.

Due to the lack of clinical data drotaverine not recommended during lactation (breast-feeding).

Cautions

The composition includes tablets 52 Lactose mg, therefore the drug in tablet form for patients not assigned with lactase deficiency, galactosemia syndrome or impaired absorption of glucose / galactose.

The composition of the solution for in / in / m administration include sodium bisulfite, which can cause allergic reactions, including anaphylaxis and bronchospasm, in susceptible individuals (especially in patients with bronchial asthma or a history of allergic reactions). If you are sensitive to sodium metabisulfite parenteral administration of the drug should be avoided.

Effects on ability to drive vehicles and management mechanisms

When administered in therapeutic doses drotaverine not affect the ability for classes of potentially hazardous activities.

After parenteral (especially in /) administration to refrain from driving motor vehicles and management mechanisms for 1 no (after application).

Overdose

So far, cases of drug overdose Nospanum^® not reported.

Drug Interactions

At simultaneous application But-spa^® may reduce the effect of levodopa antiparkinsonian.

Conditions of supply of pharmacies

The drug is in the form of a solution for / and / m introduction by prescription.

The drug is in the form of tablets is approved for use as a means of non-prescription.

Conditions and terms

Tablets in a blister should be kept at a temperature no higher than 30 ° C.

Tablets in a polypropylene vial and solution in / in / m introduction should be kept in the dark, inaccessible to children at temperature from 15 ° to 25 ° C. Shelf life – 5 years.